CAS: 1154028-82-6; 2-(6-Morpholin-4-Ylpyrimidin-4-yl)-4-(Triazol-1-yl)-1H-Pyrazol-3-One

该化合物是一种小分子药物,主要用于治疗与慢性肾病有关的贫血症(CKD),它作为一种低缺氧-可摄性因素作用,它通过稳定缺氧诱导因素(HIFs)并随后促进红血杆菌的生产,增强红血杆菌,从而稳定缺氧诱因(HIFs),从而增强红血杆菌,这一机制模仿了对低氧水平的生理反应,从而刺激了红血细胞的生产. 灰尘的特点是,它能够提高血红蛋白水平,而无需外部的EPO管理.该物质通常通过口服进行,并在各种临床试验中研究其功效和安全情况.其致癌性表明一种中度半衰期,允许病人一次性服用.与任何药物一样,潜在的副作用可能包括高血压和胃肠紊乱,从而在治疗期间需要监测.

结构式图片

欧盟法规

C&L通报

合成工艺路线路线简述

    📜4-(6-肼基-嘧啶-4-基)-吗啉,Methyl 3-(Dimethylamino)-2-(1H-1,2,3-Triazol-1-yl)Acrylate置于4-(6-肼基-嘧啶-4-基)-吗啉体系中,用84.9的收率获得1,2-二氢-2-[6-(4-吗啉基)-4-嘧啶基]-4-(1H-1,2,3-三唑-1-基)-3H-吡唑-3-一
    参考文献:Method For The Preparation Of Triazole Compounds
    标题:Method For The Preparation Of Triazole Compounds
    摘要:本发明涉及一种制备1-[6-(吗啉-4-基)嘧啶-4-基]-4-(1H-1,2,3-三唑-1-基)-1H-吡唑-5-醇(I-烯醇形式)或2-[6-(吗啉-4-基)嘧啶-4-基]-4-(1H-1,2,3-三唑-1-基)-1,2-二氢-3H-吡唑-3-酮(I-酮形式)和钠1-[6-(吗啉-4-基)嘧啶-4-基]-4-(1H-1,2,3-三唑-1-基)-1H-吡唑-5-Olate(II)的方法,从1,2,3-三唑(III),溴乙酸甲酯(Iv-Me-Br)或溴乙酸乙酯(Iv-Et-Br),4,6-二氯嘧啶(Viii),吗啉(Ix)和肼(Xii)中得到.

    海关参考信息

    专利信息


    专利号:US-10906888-B2
    优先权日:2016-07-14
    标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-10308615-B2
    优先权日:2015-05-29
    标 题:Heterocyclic compounds as inhibitors of Vanin-1 enzyme
    发明人:CASIMIRO-GARCIA AGUSTIN; CONDON JEFFREY SCOTT; FLICK ANDREW CHRISTOPHER; GOPALSAMY ARIAMALA; KIRINCICH STEVEN J; MATHIAS JOHN PAUL; STROBACH JOSEPH WALTER; XIANG JASON SHAOYUN; XING LI HUANG; WANG XIAOLUN
    权利人:PFIZER
    摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

    专利号:US-2024208898-A1
    优先权日:2021-03-25
    标 题 :Enamine n-oxides: synthesis and application to hypoxia-responsive prodrugs and imaging agents
    发明人:KIM JUSTIN; KANG DAHYE; CHEUNG SHELDON T
    权利人:DANA FARBER CANCER INST INC
    摘要:Disclosed are compounds and pharmaceutically acceptable salts and stereoisomers thereof that are suitable for diagnosis and the treatment of diseases and disorders characterized by, associate with or which exhibit tissue hypoxia, such as, for example, solid tumors. Also disclosed are pharmaceutical compositions containing same, and methods of making and using the compounds.

    专利号:US-10316018-B2
    优先权日:2015-08-27
    标题 :Bicyclic-fused heteroaryl or aryl compounds as IRAK4 modulators
    发明人:LEE KATHERINE LIN; ALLAIS CHRISTOPHE PHILIPPE; DEHNHARDT CHRISTOPH MARTIN; GAVRIN LORI KRIM; HAN SEUNGIL; HEPWORTH DAVID; LEE ARTHUR; LOVERING FRANK ELDRIDGE; MATHIAS JOHN PAUL; OWEN DAFYDD RHYS; PAPAIOANNOU NIKOLAOS; SAIAH EDDINE; STROHBACH JOSEPH WALTER; TRZUPEK JOHN DAVID; WRIGHT STEPHEN WAYNE; ZAPF CHRISTOPH WOLFGANG
    权利人:PFIZER
    摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

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    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Schmidt F, Ringeisen H, Fent G, Langston C, Collins R, Charles S. Effectiveness and long-term safety of repeated oral administrations of molidustat in the management of anemia associated with chronic kidney disease in cats. J Vet Intern Med. 2026 Jan 21;40(1):aalaf079. doi: 10.1093/jvimsj/aalaf079.
    2: Mangold-Gehring S, Hofmann S, Rouenhoff S, Schmidt F. EXPRESS: Palatability of sunflower oil-based versus aqueous verum formulations of molidustat in healthy cats. J Feline Med Surg. 2026 Feb
    20:1098612X261428943. doi: 10.1177/1098612X261428943. Epub ahead of print. 17(5):647-654. doi: 10.1002/dta.3771. Epub 2024 Jul 11.

    合成参考文献


    摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026).
    参考文献:10.1021/acs.jmedchem.7b01686
    摘要:Joharapurkar AA, Pandya VB, Patel VJ, Desai RC, Jain MR. Prolyl Hydroxylase Inhibitors: A Breakthrough in the Therapy of Anemia Associated with Chronic Diseases. J Med Chem. 2018 Aug 23;61(16):6964–82. doi: 10.1021/acs.jmedchem.7b01686.
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